156790-79-3Relevant academic research and scientific papers
INHIBITORS OF TYROSINE KINASES
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Page 52, (2008/06/13)
The invention relates to compounds of formula (I) Wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such disease.
Potent and selective inhibitors of the Abl-kinase: Phenylaminopyrimidine (PAP) derivatives
Zimmermann, Juerg,Buchdunger, Elisabeth,Mett, Helmut,Meyer, Thomas,Lydon, Nicholas B.
, p. 187 - 192 (2007/10/03)
Due to its relatively clear etiology, chronic myelogenous leukemia (CML) represents an ideal disease target for a therapy using a selective inhibitor of the Bcr-Abl tyrosine protein kinase. Extensive optimization of the class of phenylamino-pyrimidines yielded highly potent and selective Bcr-Abl kinase inhibitors. Compound 1 shows high potency (IC50 = 38 nM) and selectivity for the Abl tyrosine protein kinase at the in vitro level.
